Assay Detail
Binding
CHEMBL2393735
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Inhibition of human JNK1alpha1 using GST-tagged ATF2 as substrate preincubated for 10 mins prior to substrate addition measured after 30 mins by microplate scintillation counting analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.01 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2392833 | — | — | 1 | 8.52 |
| CHEMBL2392825 | — | — | 1 | 8.52 |
| CHEMBL2392827 | — | — | 1 | 8.30 |
| CHEMBL2392832 | — | — | 1 | 8.22 |
| CHEMBL2390974 | — | — | 1 | 8.21 |
| CHEMBL2392831 | — | — | 1 | 8.17 |
| CHEMBL2392834 | — | — | 1 | 8.15 |
| CHEMBL2392837 | — | — | 1 | 8.15 |
| CHEMBL2392838 | — | — | 1 | 8.10 |
| CHEMBL2392828 | — | — | 1 | 8.00 |
| CHEMBL2392835 | — | — | 1 | 7.92 |
| CHEMBL2392839 | — | — | 1 | 7.92 |
| CHEMBL2392826 | — | — | 1 | 7.54 |
| CHEMBL2392830 | — | — | 1 | 7.36 |
| CHEMBL2392829 | — | — | 1 | 7.03 |
| CHEMBL2392836 | — | — | 1 | - |
| CHEMBL2392840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2392833 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2392825 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2392827 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2392832 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2390974 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2392831 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2392834 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2392837 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2392838 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2392828 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2392835 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2392839 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2392826 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2392830 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2392829 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2392836 | — | IC50 | - | — | - | |
| CHEMBL2392840 | — | IC50 | - | — | - |